期刊
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
卷 55, 期 9, 页码 3153-3157出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201510743
关键词
alkylation; anilines; C-H activation; nickel; reaction mechanisms
资金
- European Research Council under the European Community's Seventh Framework Program (FP7
- ERC) [307535]
- CSC
- DFG [SPP 1807]
The C-H alkylation of aniline derivatives with both primary and secondary alkyl halides was achieved with a versatile nickel catalyst of a vicinal diamine ligand. Step-economic access to functionalized 2-pyrimidyl anilines, key structural motifs in anticancer drugs, is thus provided. The C-H functionalization proceeded through facile C-H activation and SET-type C-X bond cleavage with the assistance of a monodentate directing group, which could be removed in a traceless fashion.
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